- Synthesis, evaluation, molecular docking, and molecular dynamics studies of novel N-(4-[pyridin-2-yloxy]benzyl)arylamine derivatives as potential antitubercular agents
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A new series of novel triclosan (2,4,4′-trichloro-2′-hydroxydiphenylether) analogues were designed, synthesized, and screened for their in vitro antimycobacterial and antibacterial activities. Most of the compounds showed significant activity against Myco
- Verma, Ruchi,Boshoff, Helena I. M.,Arora, Kriti,Bairy, Indira,Tiwari, Mradul,Varadaraj, Bhat G.,Shenoy, G. Gautham
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- Design and synthesis of novel N-(4-(Pyridin-2-yloxy)benzylidene)-4-[4-(substituted)phenyl]semicarbazides as potential anticonvulsant agents
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A new series of N-(4-(pyridin-2-yloxy)benzylidene)-4-[4-(substituted)phenyl]semicarbazides (PSSD1-8) were designed and synthesized keeping in view the structural requirement of pharmacophore and evaluated for their possible anticonvulsant activity. All the derivatives were synthesized by the given scheme and reaction process was monitored by thin layer chromatography. The structure of synthesized derivatives was confirmed by FT-IR, 1H NMR, mass spectroscopy and elemental analysis. The anticonvulsant activity was established after intraperitoneal administration in MES and scMET seizure models. The most active compound of the series was 1-(4-(pyridin-2-yloxy)-benzylidene)-4-p-tolylsemicarbazide (PSSD5). A molecular docking study was carried out in order to assess the interaction and binding modes with target receptor/enzyme. Titled compounds were found to strongly bind to human gamma-aminobutyric acid receptor (GABAAR-β3). A computational study was also carried to predict the pharmacokinetic properties of the synthesized compounds.
- Singh, Prem,Tripathi, Laxmi
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p. 2193 - 2200
(2018/09/10)
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- Highly efficient copper-catalyzed O-arylation using readily available (S)-N-methylpyrrolidine-2-carboxamide as the ligand
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A highly efficient and readily available catalyst system for O-arylation of various phenols using CuI and (S)-N-methylpyrrolidine-2-carboxamide (Pro-NHMe) was developed. The reaction is widely applicable to the synthesis of diaryl ethers. Georg Thieme Verlag Stuttgart.
- Liu, Xianghao,Fu, Hua,Jiang, Yuyang,Zhao, Yufen
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p. 221 - 224
(2008/09/21)
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- PROCESSES FOR PREPATING N-(SUBSTITUTED ARYLMETHYL)-4-(DISUBSTITUTED METHYL)PIPERIDINES AND INTERMEDIATES
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I Improved processes are described for preparing compounds of formulae: (B, C, F, H) wherein R1, R2, B and Z are defined herein. These compounds are useful in the preparation of N-(substituted arylmethyl)-4-(disubstituted methyl)piperidines.
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Page/Page column 10-12
(2008/06/13)
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- Substituted aromatic ethers as inhibitors of glycine transport
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This invention relates to a series of substituted aromatic ethers of the formula I wherein ring A and X and Y are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutic
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- Insecticidal N-heterocyclylalkyl-or N-[(polycyclyl)alkyl]-N′substituted piperazines
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Compounds of the following structure are disclosed as effective insecticides: in which: A and B are independently lower alkyl; U is lower alkylidene, lower alkenylidene, or CH—Z, where Z is hydrogen, lower alkyl, lower cycloalkyl, or phenyl; R is phenyl o
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